Compositions for the prophylaxis and treatment of dermatological/mucosal diseases, and uses thereof

Abstract

The present invention provides a composition containing a) clay material with a negative surface charge; b) magnesium ions and calcium ions both either incorporated within the clay material and / or added separately; c) water and / or non-aqueous solvent; d) substantially non-cationic carrier; where i) the mean particle size of the clay material is at least 5 nm; and ii) the total molar amount of magnesium ions is higher than the total molar amount of calcium ions. The present invention further relates to the use of said composition in the manufacture of a medicament for the prophylaxis and treatment of skin diseases, skin conditions, or mucosal diseases where the formation and / or recovery of epidermal / mucosal barrier function has beneficial effects.

Description

FIELD OF THE INVENTION[0001]The present invention relates to compositions for the prophylaxis and treatment of dermatological and mucosal diseases / disorders. In particular, the present invention relates to novel compositions for the prophylaxis and treatment of dermatological diseases / disorders, skin conditions, and mucosal diseases / disorders where epidermal / mucosal barrier formation and / or recovery would have beneficial effects. The invention further relates to the use of such compositions in the manufacture of medicaments / medical devices / care products for the prophylaxis and treatment of said diseases.BACKGROUND OF THE INVENTION[0002]The outermost layer of the skin is the epidermis and the mucosal membranes (e.g. buccal, nasal, intestinal, anal) which forms a barrier between the body and the external environment. This semipermeable epidermal barrier prevents both the escape of moisture and the entry of infectious or toxic substances. Common inflammatory skin disorders such as atop...

AI Technical Summary

Benefits of technology

[0031]We have surprisingly found that a composition that is able to form an electric double layer in aqueous or non-aqueous medium, and shows a stable negative charge, has a cation exchange capacity and cation binding capacity, furthermore contains total magnesium ions more than the total amount of calcium ions, in combination with a non-ionic, anionic, amphoteric or very weakly cationic carrier, is able to recover damaged epidermal barrier upon topical application on the affected skin area.

[0032]A negative charge can be formed by any natural or artificial clay material with a negative surface charge. Zeolites, especially clinoptilolite are the preferred choice of clay material according to the present invention. The clay material is preferably in the form of small particles (micronized particles), since this average size range provides acceptable small particles to be applicable on skin surface, and acceptable high specific surface and charge. According to the present invention the minimal average clay particle size is 5 nm, —the applied particle size depends on the surface type and the status of its barrier damage—, which can make sure that the composition does not penetrate through the skin / into the blood stream, therefore can remain on the skin surface for a time period which is necessary for the desired therapeutic effect.

[0034]The presence of calcium ions in the composition of the invention is also necessary. Calcium assists exocytosis of the lamellar granules in stratum granulosum and induces terminal differentiation of stratum corneum, formation of cornified envelope and also epidermal lipid synthesis. After extrusion of lamellar granules content, the applied ionic environment contribute for the stacks of membranes to reorganize structurally, to form patterned lamellar sheets via edge-to-edge fusion of the lipid stacks. Calcium also activates the trans-glutaminase enzyme to irreversibly cross-link the cornefied envelope proteins, creating a tough insoluble sac that surrounds the keratin fibers.

[0036]According to the present invention, the composition should be able to form an electric double layer in aqueous or non-aqueous medium, and should provide a stable negative charge.

Problems solved by technology

The further problem with dolomite is its nickel content, which is undesired in most of said dermatological diseases.

However, the main drawback of these medical formulations is the pH of the formulations that is far from the skin-neutral value (which is about pH 5.5).

The strongly basic or acidic character of these formulations might result in irritation and in slower recovery of the skin diseases to be treated.

Moreover, one can not reproduce these formulations, since the exact Ca:Mg ratio is not clearly defined in the description.

To summarize, the problem with the formulations according to this prior art document is that it either relates to a silicium dioxide carrier with calcium carbonate and magnesium carbonate, however, the pH of these formulations is undesired, or zeolite is mentioned together with dolomit, however, here the calcium to magnesium ratio is not defined.

Although the agent according to this state of the art document comprises calcium and / or magnesium ions, the drawback of this formulation is that it does not necessarily contain both of them.

Although the role of the epidermal barrier was recognized in several skin diseases / disorders, according to the state of the art there is no pharmaceutical / cosmetic composition available that were optimized to the finding according to which these skin diseases could be treated by epidermal skin barrier formation and / or recovery.